Tenofovir hydrate

Category	Human immunodeficiency Virus (HIV)
CAS	206184-49-8
Description	Tenofovir(GS 1278, PMPA) is an antiretroviral drug known as nucleotide analogue reverse transcriptase inhibitors (NRTIs), which block reverse transcriptase, a crucial virus enzyme in HIV-1 and HBV.

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Product Information

Synonyms	Viread hydrate; GS 1278 hydrate; GS1278 hydrate; GS-1278 hydrate; PMPA hydrate; TDF hydrate
IUPAC Name	[(2R)-1-(6-aminopurin-9-yl)propan-2-yl]oxymethylphosphonic acid;hydrate
Molecular Weight	305.23
Molecular Formula	C9H16N5O5P
Canonical SMILES	CC(CN1C=NC2=C1N=CN=C2N)OCP(=O)(O)O.O
InChI	InChI=1S/C9H14N5O4P.H2O/c1-6(18-5-19(15,16)17)2-14-4-13-7-8(10)11-3-12-9(7)14;/h3-4,6H,2,5H2,1H3,(H2,10,11,12)(H2,15,16,17);1H2/t6-;/m1./s1
InChIKey	PINIEAOMWQJGBW-FYZOBXCZSA-N
Boiling Point	616.1°C at 760mmHg
Flash Point	326.4°C
Purity	>98%
Density	1.79g/cm3
Solubility	DMSO : ≥ 6 mg/mL (19.66 mM)
Appearance	White to off-white (Solid)
Application	Anti-HIV Agents
Storage	4°C, stored under nitrogen * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Complexity	354
Exact Mass	305.08890563
In Vitro	Tenofovir shows cytotoxic effects on cell viability in HK-2 cells, with IC50 values of 9.21 and 2.77 μM at 48 and 72 h in MTT assay, respectively. Tenofovir diminishes ATP levels in HK-2 cells. Tenofovir (3.0 to 28.8 μM) increases oxidative stress and protein carbonylation in HK-2 cells. Furthermore, Tenofovir induces Apoptosis in HK-2 cells, and that Apoptosis is induced via mitochondrial damage. Tenofovir and M48U1 formulated in 0.25% HEC each inhibits the replication of both R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs, and inhibits several laboratory strains and patient-derived HIV-1 isolates. The combined formulation of M48U1 and tenofovir in 0.25% HEC exhibits synergistic antiretroviral activity against infection with R5-tropic HIV-1BaL, and is not toxic to PBMCs.
PSA	155.42000
Target	HIV; Reverse Transcriptase